Sunitinib Malate

Licensed by Pfizer Catalog No.S1042

Sunitinib Malate Chemical Structure

Molecular Weight(MW): 532.56

Sunitinib Malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit.

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In DMSO USD 191 In stock
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USD 147 In stock
USD 447 In stock
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Cited by 42 Publications

12 Customer Reviews

  • PDGF-AA induces Ezh2 expression and proliferation in juvenile islets but not in adult islets. Western immunoblots of indicated islet proteins from 3 week or 9 month-old WT islets 2 days after exposure to PDGF-AA alone, or PDGF-AA plus RTK inhibitors Sunitinib.

    Nature 2011 478(7369):349-55. Sunitinib Malate purchased from Selleck.

    Assessment of effects on human juvenile or adult islets after exposure to PDGF-AA (50 ng/ml) for 2 days, with or without Sunitinib (2 uM) or U0126 (10 uM)co-treatment. Average percentage of BrdU+ insulin+ cells was morphometry from sectioned islets immunostained for insulin (green), glucagon (white) and BrdU (red). n = 3-6 independent experiments.

    Nature 2011 478(7369):349-55. Sunitinib Malate purchased from Selleck.

  • Combinational treatment of kinase inhibitors induces the similar phenotype produced by PP1. All images are lateral view with dorsal to the top and anterior to the left. The combinational treatment of Dasatinib (D) or U0126 (U) with Sunitinib (SU),PTK787 (PTK), or ZM323881 (Z) resulted in the shrinkage of dorsal aorta.

    Cell Res 2011 21, 1080-1087. Sunitinib Malate purchased from Selleck.

    A, Tumor growth curves from the initial sunitinib drug trials, with endpoint set at 1,300 mm3 (mean ± SEM). Measurements began one week after tumor inoculation and on the day sunitinib treatment began. Subsequent experimental endpoints were set on the basis of these growth curves and their intersections with this data are shown. B, Histogram plot showing the distribution of tumor sizes at day 8 of treatment. Sunitinib-treated tumors exceeding 250 mm3 in size were identified as falling into the nonresponsive cohort. Sunitinib treatment significantly retards growth of responsive tumors.

    Cancer Res, 2017, 77(4):1008-1020 . Sunitinib Malate purchased from Selleck.

  • Sunitinib decreases FLT-3 and RET phosphor ylation but increases ERK phosphorylation in a time-dependent manner. H295R and SW13 cells were treated with sunitinib (10 nM) for various time points as indi-cated. Cell lysates were prepared and phospho-FLT-3, RET, and ERK levels were monitored by Western Blot-ting. Re-probing against FLT-3, RET, and ERK was done to ensure equal protein loading.

    Surgery 2012 152, 1045-50. Sunitinib Malate purchased from Selleck.

    Sunitinib or PD98059 decreases cell proliferation in a dose-dependent manner. H295R and SW13 cells were treated with various concentration of sunitinib or PD98059 for 48 hours as indicated. Treated cells were subjected to the MTS proliferation assay. Similar experiments were repeated 3 times. Histograms represent relative % of OD490 nm absorbance (* P < .05). All data are relative multiples of expression compared with untreated cells. The data are representative of three experiments and are expressed as the mean ?SE.

    Surgery 2012 152, 1045-50. Sunitinib Malate purchased from Selleck.

  • Autophagic activation in sunitinib- and sorafenib- but not AZD6244-treated cells. Medullary thyroid cancer-1.1 (MTC-1.1; A) and TT ( B) cells were treated with dimethyl sulfoxide (DMSO), sunitinib (50 nM), sorafenib (10 nM), AZD6244 (30 nM), or everolimus (20 nM) for 48 hours. Cell lysates were prepared, and light chain 3 (LC3)-I and -II cleaved caspase-3 protein levels were monitored by Western blotting. Reprobing against actin was per formed to ensure equal protein loading. ( C ) MTC-1.1 and TT cells were transiently transfected with autophagy protein 5 (Atg-5) small inter fering RNA. Transfection with scrambled small inter fering RNA was used as a control. After transfection, cells with and without Atg-5 knockdown were exposed to DMSO or 20 nM of everolimus for 48 hours. Cell lysates were pre- pared and LC3-I and -II protein expression levels were monitored by Western blotting. Reprobing against Atg-5 was per formed to monitor Atg-5 knockdown efficiency. Reprobing against actin was per formed to ensure equal protein.

    Surgery 2012 152, 1142-9. Sunitinib Malate purchased from Selleck.

    Autophagy inhibition blocks the antiproliferative effects of sunitinib and sorafenib but not AZD6244. Medullary thyroid cancer–1.1 (MTC-1.1) and TT cells were transfected transiently with scrambled or autophagy protein 5 (Atg-5) small inter fering RNA. After transfection, cells with and without Atg-5 knockdown were exposed to sunitinib (50 nM), sorafenib (10 nM), and AZD6244 (30 nM) for 48 hours. Treated cells were subjected to a 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium proliferation assay. Similar experiments were repeated 3 times. Histograms represent the relative percent of OD490 nM absorbance. The asterisk indicates significance versus scrambled small inter fering RNA–treated control ( P < .05). All data are relative multiples of expression compared to untreated cells. The data are representative of 3 experiments and are expressed as the mean ± the standard error.

    Surgery 2012 152, 1142-9. Sunitinib Malate purchased from Selleck.

  • Sunitinib limits the colonial growth of HT-29 by downregulating HIF-1a. (A) The number and size of colonies formed in soft agar. The numbers of small colonies (<50 μm diameter) were not different among conditions of a serial concentration of sunitinib. On the contrary, large colonies (>50 μm diameter) disappeared after incubation with sunitinib. Each point represents the mean and SD from four separate experiments. (B) HIF-1a expression and hypoxia within HT-29 colony. After colonies grew for 4 weeks, HIF-1a and hypoxia were visualized by immunofluoroscence staining. Bar = 20 μm.

    Biochem Bioph Res Co 2010 398, 205–211. Sunitinib Malate purchased from Selleck.

    2. Sunitinib downregulates HIF-1a. (A) Dose-dependent repression of HIF-1a protein level by sunitinib in HT-29. HT-29 cells were incubated under normoxic (N) or hypoxic (H) conditions in the presence of sunitinib for 24 h. HIF-1a and ARNT proteins in total cell lysates were analyzed by Western blotting. (B) Sunitinib attenuates the hypoxic induction of HIF-1 target genes. RNAs were isolated from HT-29 cells subjected to normoxia (N) or hypoxia (H) in the presence of sunitinib for 16 h. The mRNAs of HIF-1a and its target genes were analyzed by RT-PCR and autoradiography. PGK1 indicates phosphoglycerate kinase 1; PDK1, pyruvate dyhydrogenase kinase 1; CAIX, carbonic anhydrase IX. (C) Sunitinib-induced HIF-1 inhibition. Epo-enhancer and b- galactosidase reporter plasmids were co-transfected into HEK293 cells. After 16 h incubation, luciferase and b-galactosidase activities were measured. *P < .05 versus the hypoxic control.

     

     

    Biochem Bioph Res Co 2010 398, 205–211. Sunitinib Malate purchased from Selleck.

  • Sunitinib inhibits 50-UTR-dependent translation of HIF-1a. (A) 50 cap-dependent translational activity of HIF-1a. The luciferase reporter plasmid contains the HIF-1a 50-UTR segment between the tk promoter and the luciferase gene. HT-29 cells were co-transfected with the reporter plasmid (8 lg per 100-mm dish) and the b-gal plasmid (4 μg). After 16 h incubation under normoxic or hypoxic conditions with sunitinib, cells were lysed and subjected to luciferase assay. *P < .05 versus the hypoxic control. (B) IRES-dependent translational activity of HIF-1a. The luciferase reporter plasmid contains the HIF-1a 50-UTR segment between the GFP gene and the luciferase gene. HT-29 cells were co-transfected with the reporter plasmid (8 μg) and the b-gal plasmid (4 μg). *P < .05 versus the hypoxic control. (C) Sunitinib inhibits phosphorylation of Akt. After 8 h incubation under hypoxic condition with sunitinib, HT-29 cells were lysed and subjected to Western blotting. (D) Sunitinib suppresses HIF-1a in VHL-null RCC4 cells. VHL (-/-) RCC4 cells were incubated under normoxic conditions sunitinib for 8 h, and HIF-1a in total cell lysates was analyzed by Western blotting.

     

     

    Biochem Bioph Res Co 2010 398, 205–211. Sunitinib Malate purchased from Selleck.

    Experimental layout for VEGF signaling blocking and LCMV infection in WT mice. Mice received two injections on day 0 and 3 p.i. of Abs as described in Material and Methods, or daily gavage of the VEGFR/PDGFR-inhibitor sunitinib. Inguinal LN volume on day 0 (D0) or day 8 (D8) p.i. after treatment of mice with control Ig or anti-VEGFR2, anti-VEGF-A Abs or sunitinib. Pooled from 1-2 independent experiments with 3-5 mice per treatment. D. Total HEV length on day 0 (D0) or day 8 (D8) p.i. as in C. No significant difference was found in C and D between day 8 control Ig and Ab- or inhibitor-treated values (One-way ANOVA).

    AACR Sunitinib Malate purchased from Selleck.

Purity & Quality Control

Choose Selective PDGFR Inhibitors

Biological Activity

Description Sunitinib Malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit.
Targets
Kit [1]
(Cell-free assay)
FLT3 [1]
(Cell-free assay)
PDGFRβ [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
FGFR1 [1]
(Cell-free assay)
2 nM 80 nM 2.9 μM
In vitro

Sunitinib also potently inhibits Kit and FLT-3. [1] Sunitinib is a potent ATP-competitive inhibitor of VEGFR2 (Flk1) and PDGFRβ with Ki of 9 nM and 8 nM, respectively, displaying >10-fold higher selectivity for VEGFR2 and PDGFR than FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, and src. In serum-starved NIH-3T3 cells expressing VEGFR2 or PDGFRβ, Sunitinib inhibits VEGF-dependent VEGFR2 phosphorylation and PDGF-dependent PDGFRβ phosphorylation with IC50 of 10 nM and 10 nM, respectively. Sunitinib inhibits VEGF-induced proliferation of serum-starved HUVECs with IC50 of 40 nM, and inhibits PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRβ or PDGFRα with IC50 of 39 nM and 69 nM, respectively. [2] Sunitinib inhibits phosphorylation of wild-type FLT3, FLT3-ITD, and FLT3-Asp835 with IC50 of 250 nM, 50 nM, and 30 nM, respectively. Sunitinib inhibits the proliferation of MV4;11 and OC1-AML5 cells with IC50 of 8 nM and 14 nM, respectively, and induces apoptosis in a dose-dependent manner. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
3T3 M3foNWtqdmG|ZTDBd5NigQ>? NHvRZZFKdmirYnn0bY9vKG:oIGDES2YucW6mdXPl[EBDemSXIHnuZ49zeG:{YYTpc44hf2m2aDDJR|UxKG:oIECuNFA4KM7:TR?= NVfaVXFoOTJ4NE[wNVk>
3T3 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HhVGlvcGmkaYTpc44hd2ZiUHzheIVt\XRvZHXybZZm\CCpcn;3eIgh\mGldH;yJIlv\HWlZXSgN3Q{KGOnbHygdJJwdGmoZYLheIlwdiC5aYToJGlEPTBib3[gNE4xOSEQvF2= MXOxNlY1PjBzOR?=
3T3 NXj6cpdnTnWwY4Tpc44hSXO|YYm= NEPhN3RKdmirYnn0bY9vKG:oIG\hd4N2dGG{IHXu[I91cGWuaXHsJIdzd3e2aDDmZYN1d3JicnXj[ZB1d3Jid3n0bEBKSzVyIH;mJFAvODVizszN MmjPNVI3PDZyMUm=
3T3 MmHkT4lv[XOnIFHzd4F6 MVSyNEBucW5? NXPWO5VwTE2VTx?= M4S0W2NmdGy3bHHyJIlvcGmkaYTpc44hd2ZiVlXHSkBqdmS3Y3XkJIh2dWGwIFvEVkBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEKyJO69VQ>? M1vqNFE3OTZ{MEC4
NIH3T3 M3\KeWtqdmG|ZTDBd5NigQ>? M3XoRlIxKG2rbh?= M1zyeGROW09? MYHpcohq[mm2IHj1cYFvKEuGUjDrbY5ie2ViZYjwdoV{e2WmIIfpeIghUUN3MDDv[kAxNjBzODFOwG0> MljrNVYyPjJyMEi=
A549 NHzZO|dHfW6ldHnvckBCe3OjeR?= MljLSG1UVw>? M1fEPGlvcGmkaYTpc44hd2ZiYz3N[ZQh\GWyZX7k[Y51KEiJRj3pcoR2[2WmIHj1cYFvKEF3NEmgZ4VtdCCvaXfyZZRqd25id3n0bEBKSzVyIH;mJFIh|ryP MXKxPFQ{PDF2NR?=
DU145 MmnPSpVv[3Srb36gRZN{[Xl? MXfEUXNQ NIG5VWhKdmirYnn0bY9vKG:oIHOtUYV1KGSncHXu[IVvfCCKR1[tbY5lfWOnZDDoeY1idiCGVUG0OUBk\WyuIIPjZZR1\XKrbnege4l1cCCLQ{WwJI9nKDFyIN88US=> M33ReFE5PDN2MUS1
KB3-1 NUX1O4hZS3m2b4TvfIlkKEG|c3H5 NX7Jfm01PzJiaB?= MoTiSG1UVw>? NH3kXVREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRNWeyLX7l[4F1cX[nIFvCMVMuOSClZXzsd{B4cXSqIFnDOVAhd2ZiMj6zJO69VQ>? MkLTNVk{QTd|MkK=
KBV1 NHzvdYhEgXSxdH;4bYMhSXO|YYm= MX:3NkBp NU\aXmJ{TE2VTx?= Ml7NR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVE1odHmlb4Dyc5RmcW5vZYjwdoV{e2mwZzDLRnYyKGOnbHzzJJdqfGhiSVO1NEBw\iB2LkGg{txO MV6xPVM6PzN{Mh?=
A375 MV\DfZRwfG:6aXOgRZN{[Xl? M4\UfVczKGh? M3PkZWROW09? M{TUUmlEPTB;NT60JO69VQ>? NH\5OlQyQTZ3NESwPC=>
RS4-11 NYDYSmR5TnWwY4Tpc44hSXO|YYm= NVXKeYZrOiCq M2TY[mlvcGmkaYTpc44hd2ZiRlzUN{BifXSxcHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCwMlAxQTlizszN NEjhe3MyQTZ3NESwPC=>
RS4-11 MnvZSpVv[3Srb36gRZN{[Xl? MkX1NkBp M4PHfWlvcGmkaYTpc44hd2ZiRlzUN{BKXERibYX0ZY51KGG3dH;wbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvODN2IN88US=> NGq1eHUyQTZ3NESwPC=>
Sf9 NV\LdJBKU2mwYYPlJGF{e2G7 M4DvUlMxKG2rbh?= M3;QbWlvcGmkaYTpc44hd2ZiR2PUMZRi\2enZDDWSWdHWiCneIDy[ZN{\WRid3n0bEBKSzVyIH;mJFAvOTh3IN88US=> NGLPToQyQTh3NEC1NS=>
Ba/F3 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjvbok4OiCq NH\IfohKSzVyPUGuNkDPxE1? MkixNlAyOTdyMES=
BaPTC2 M4HRXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWj4UGE6PzJiaB?= M3zHcmlEPTB;MD6yNkDPxE1? M164W|IxOTF5MEC0
Sf9 NVnLOJh6TnWwY4Tpc44hSXO|YYm= Mn3sNUBp NHvqfo1FVVOR MYPJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KEircz30ZYdo\WRiUlXUJIV5eHKnc4Pl[EB4cXSqIFnDOVAhd2ZiMT6zJO69VQ>? Mn7sNlAyOTdyMES=
H4 M3rSNWN6fG:2b4jpZ{BCe3OjeR?= Mnn2NVAh|ryP M32wU3RwgGmlaYT5JIlvKGi3bXHuJGg1KGOnbHzz NHPieFUzODN3MEiwOi=>
SF-539 NWfHNFlCU2mwYYPlJGF{e2G7 M4XneFM{OyEQvF2= NUX0U5JYPjBibXnu MnKzSG1UVw>? NVfuR2d{UW6qaXLpeIlwdiCxZjDQSGdHWmKndHGgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAyOi5{IN88US=> NWexT5M6OjB2MEO3NFA>
U251 NWmzWnpRU2mwYYPlJGF{e2G7 MlH6N|M{KM7:TR?= NYG4c255PjBibXnu NF3INJRFVVOR M3H0W2lvcGmkaYTpc44hd2ZiVlXHSnIzKHCqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMUiuPUDPxE1? NFvNc4UzODRyM{ewNC=>
A431 MXfLbY5ie2ViQYPzZZk> NEXOSWVKdmirYnn0bY9vKG:oIGDES2ZT[mW2YTDlfJBz\XO|ZXSge4l1cCCLQ{WwJI9nKDF{LkKg{txO M1fjWVIxPTV6MEey
A431 NGLqSW9McW6jc3WgRZN{[Xl? MUPJcohq[mm2aX;uJI9nKF[HR1\SNkBmgHC{ZYPz[YQhf2m2aDDJR|UxKG:oIEG4Mlkh|ryP NWDxZWhkOjB3NUiwO|I>
HepG2 NWL3XGJ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTJeXNJPzJiaB?= NELJb|VKSzVyPUOuPFEh|ryP MoH4NlA2PzB3Mk[=
Kasumi-1 MmC4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVi3NkBp MmXlTWM2OD1yLkCxOkDPxE1? NGrWcIQzODV5MEWyOi=>
RS4-11 MlexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTGdlltPzJiaB?= M4PiTWlEPTB;MTFOwG0> MUeyNFU4ODV{Nh?=
THP1 NU\zUVFuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfVS3U4OiCq NIfLbpBKSzVyPUCuOUDPxE1? NIDRSXEzODV5MEWyOi=>
Kasumi-1 MljUSpVv[3Srb36gRZN{[Xl? Mn3ETY5pcWKrdHnvckBw\iClLVvpeEBifXSxcHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCwMlAyPSEQvF2= MXSyNFg{OzB|OR?=
A549 NGDz[JdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX2ycYhGOTZiaB?= NIfUOFNCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzz M{[zRVIyPDVyNE[z
HL60 M2TBOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4O0WFE3KGh? MlHwRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFy2NEBk\Wyucx?= MlLvNlE1PTB2NkO=
HUVEC NVW4[3BbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUGxOkBp NYLid4s{UW6qaXLpeIlwdiCxZjDWSWdHNWmwZIXj[YQh[2WubDDwdo9tcW[ncnH0bY9vKHerdHigTWM2OCCxZjCyMlc2KM7:TR?= NIXRSoIzOTR3MES2Ny=>
HUVEC NV\JfWVXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rl[lE3KGh? NX7rc4VGUW6qaXLpeIlwdiCxZjDiSmdHNWmwZIXj[YQh[2WubDDwdo9tcW[ncnH0bY9vKHerdHigTWM2OCCxZjC0MlA1KM7:TR?= NFm4[WQzOTR3MES2Ny=>
IM9 M{PaWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\HNVYhcA>? M1q1Z2FvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFnNPUBk\Wyucx?= MmnINlE1PTB2NkO=
K562 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPzNVYhcA>? MUjBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNNU[yJINmdGy| MnjZNlE1PTB2NkO=
MDA-MB-231 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYqxOkBp MkLyRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[Yxtew>? MYKyNVQ2ODR4Mx?=
H460 NEHHZ4REgXSxdH;4bYMhSXO|YYm= NHHJe3I4OiCq MYnJR|UxRTJwNzFOwG0> NXrFO3pZOjF4MkG4PFA>
SMMC7721 NXTUZXB5S3m2b4TvfIlkKEG|c3H5 M3;2PVczKGh? MnnFTWM2OD14LkS3JO69VQ>? NVGxR5hyOjF4MkG4PFA>
WI38 NF;6c|hEgXSxdH;4bYMhSXO|YYm= MnLHO|IhcA>? MYLJR|UxRThwNU[g{txO NVS1WVl6OjF4MkG4PFA>
HEK293 MUXLbY5ie2ViQYPzZZk> MoXiNVAxKG6P MV6xJIg> NWjCSml6\G:nczDuc5QhcW6qaXLpeEBXTUeILXnu[JVk\WRiYYX0c5Bpd3OyaH;yfYxifGmxbjDv[kB1gXKxc3nu[UAyOTd3IILld4llfWVib36gWmVITlJ{IHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHN? NVvnWJhHOjF6OEWyPFc>
HUVEC NHHacIlHfW6ldHnvckBCe3OjeR?= NXLYd29IOSEQvF2= NFnRVpUzPCCq MV7BcpRq[W6paX;n[Y5q[yCjY4Tpeol1gSCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBXTUeILXnu[JVk\WRiY3XscEBucWe{YYTpc44> M2i5VlIyQTZ|M{C1
HUVEC NYHXfXEyTnWwY4Tpc44hSXO|YYm= MXGxJO69VQ>? NV7nTpp7OSCq MYXJcohq[mm2aX;uJI9nKEWUSzDwbI9{eGixconsZZRqd25iYYSgWIhzOjB{L2T5dlIxPCCrbjDWSWdHNXO2aX31cIF1\WRiSGXWSWM> Mn7kNlE6PjN|MEW=
HUVEC M1PpcWZ2dmO2aX;uJGF{e2G7 NVy3VYlOOSEQvF2= M3W2fVEhcA>? M{jXT2lvcGmkaYTpc44hd2ZiZV7PV{BxcG:|cHjvdplt[XSrb36gZZQhW2W{LUGxO|IhcW5iVlXHSk1{fGmvdXzheIVlKEiXVlXD MXyyNVk3OzNyNR?=
HUVEC MWfLbY5ie2ViQYPzZZk> MlTINUDPxE1? NHLwOJQyKGh? MnHOTY5pcWKrdHnvckBw\iCYRVfGVlIheGixc4Doc5J6dGG2aX;uJIF1KHS7cj2xNVc2KGmwIG\FS2Yue3SrbYXsZZRm\CCKVW\FRy=> MV[yNVk3OzNyNR?=
HUVEC MlHaSpVv[3Srb36gRZN{[Xl? NUPyPHJKOSEQvF2= MX2xJIg> M{X6e4Rw\XNibn;0JIlvcGmkaYSgRWtVKHCqb4PwbI9zgWyjdHnvckBifCCVZYKtOFc{KGmwIG\FS2Yue3SrbYXsZZRm\CCKVW\FRy=> MofGNlE6PjN|MEW=
HL60 NYDl[2VHS3m2b4TvfIlkKEG|c3H5 MV21NEDPxE1? NV3HRop[PDhiaB?= MV7EUXNQ NGHBcGdKSzVyPUG1MlUh|ryP MX6yNlAyQTF6OB?=
K562 M2HYe2N6fG:2b4jpZ{BCe3OjeR?= NU\iNXlRPTBizszN MX20PEBp NI\ycGdFVVOR MXfJR|UxRTJzLkmg{txO Mo\qNlIxOTlzOEi=
PC3 NW[w[WNNS3m2b4TvfIlkKEG|c3H5 MXu1NEDPxE1? M{\lNFQ5KGh? NEDpZWZFVVOR M3;COmlEPTB;MkWuNUDPxE1? MY[yNlAyQTF6OB?=
SF-539 MYDLbY5ie2ViQYPzZZk> Mly0N|M{KM7:TR?= MmjzOlAhdWmw MlfETY5pcWKrdHnvckBw\iCSRFfGVoJmfGFidInyc5NqdmVia3nuZZNmKGGldHn2bZR6KGmwIGDES2YuSkJvc4TpcZVt[XSnZDDoeY1idiCVRj21N|kh[2WubIOge4l1cCCLQ{WwJI9nKDF{LkKg{txO NFeyfWwzOjJyNEe0NS=>
HAEC MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUX6c4tWOTByIN88US=> MVW3NkBp M2DsemFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFHFR{Bk\WyuczDlfJBz\XO|aX7nJHZGT0[UIIfpeIghUUN3MDDv[kAxNjFizszN MV[yNlQ1PDZ5OR?=
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HAL-01 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTJwMEW5OFYh|ryP MoniV2FPT0WU
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OPM-2 M4fsS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkG3TWM2OD1|LkC1PVU1KM7:TR?= NFvre3NUSU6JRWK=
SF126 Ml[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHSeI9pUUN3ME2zMlA3OTl6IN88US=> MXjTRW5ITVJ?
BE-13 NVGzeGw4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3W[ZhoUUN3ME2zMlI{OTFzIN88US=> NFrke|VUSU6JRWK=
SF268 MnznS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jJZmlEPTB;Mz6zNlg3QSEQvF2= M3HjVHNCVkeHUh?=
MOLT-4 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLSTWM2OD1|LkO5PFM5KM7:TR?= M2nBVXNCVkeHUh?=
PF-382 NGX6R41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PIRWlEPTB;Mz60OFU4KM7:TR?= NITHOpFUSU6JRWK=
HEL MnrzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;QTWM2OD1|LkS4NFA2KM7:TR?= NEPwdJpUSU6JRWK=
RPMI-6666 MnvOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nJdmlEPTB;Mz61OFE4OSEQvF2= M3rFWHNCVkeHUh?=
QIMR-WIL NIXBRlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrNfYxKSzVyPUOuOlM{QTFizszN MXnTRW5ITVJ?
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HCE-4 MnX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTNwN{i2OFIh|ryP MV7TRW5ITVJ?
SK-LMS-1 MnjxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDSTWM2OD1|LkizN|M5KM7:TR?= M1W0cnNCVkeHUh?=
MS-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2m0eGlEPTB;Mz64N|c4QCEQvF2= MWLTRW5ITVJ?
JAR MlHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXkTIVtUUN3ME2zMlk5QDN{IN88US=> M{fvfHNCVkeHUh?=
KE-37 NWn5UZhRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIO5UFJKSzVyPUSuNFYyPThizszN NXnuSmFiW0GQR1XS
LB996-RCC MmDYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTRwMUKxOlgh|ryP NGDNUFNUSU6JRWK=
HH NHz3[WlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoT3TWM2OD12LkKwPVE1KM7:TR?= NHW5foxUSU6JRWK=
HL-60 NVfXdVhHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1yzVGlEPTB;ND6yNVA3PSEQvF2= M3vadHNCVkeHUh?=
HOP-62 M13Oc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HFTWlEPTB;ND6zN|UzKM7:TR?= NHfqTVFUSU6JRWK=
NOMO-1 NIHKUGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFe1ZW9KSzVyPUSuN|M3QTlizszN Ml7tV2FPT0WU
DU-4475 MnTIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYH5VZc1UUN3ME20MlM3PzJ7IN88US=> NYPETGU5W0GQR1XS
LC4-1 NHraZWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTRwM{iwO{DPxE1? MUPTRW5ITVJ?
MC116 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zGd2lEPTB;ND60N|A5OSEQvF2= NV70ellbW0GQR1XS
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SK-N-DZ MmT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITJeHlKSzVyPUSuOlcxQTlizszN MUTTRW5ITVJ?
EW-1 Ml3JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTRwNke5NVEh|ryP NWXUSI5JW0GQR1XS
SU-DHL-1 MlTRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\qOnFnUUN3ME20MlgxOTd2IN88US=> M37V[HNCVkeHUh?=
L-363 M1frdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzsTWM2OD12LkiwOlIyKM7:TR?= MX\TRW5ITVJ?
OS-RC-2 M4HqXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnwUHNUUUN3ME20Mlg4OzFizszN NXfPUY9KW0GQR1XS
HD-MY-Z NH[0N5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTVwMUezNFEh|ryP NYPYSXdQW0GQR1XS
MHH-PREB-1 MkPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrJOVlKSzVyPUWuN|I{OTJizszN MoPvV2FPT0WU
HC-1 M2fZcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTVwNEOyPVEh|ryP NHrycVRUSU6JRWK=
SK-MM-2 NUPtSnZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rEZmlEPTB;NT60O|gzKM7:TR?= M{jpcnNCVkeHUh?=
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MHH-CALL-2 NH;VcHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\h[41KSzVyPUWuO|Y4OTlizszN MmL6V2FPT0WU
KG-1 NUDNR4dJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWO2ZZRxUUN3ME22MlAzQDd6IN88US=> NWDFS4lZW0GQR1XS
J-RT3-T3-5 MmiwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\kWFRzUUN3ME22MlA4QTB7IN88US=> MWLTRW5ITVJ?
MMAC-SF NFjzOHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;1R2lEPTB;Nj6xNFk1QSEQvF2= MWTTRW5ITVJ?
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SW954 MnPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTZwMke1NVch|ryP NYnpblZ7W0GQR1XS
HDLM-2 MkTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDlTWM2OD14LkOyNVA6KM7:TR?= MV3TRW5ITVJ?
ST486 NHTHT|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTtTWM2OD14LkO0O|Eh|ryP M1vnN3NCVkeHUh?=
DG-75 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTZwNEOwOlkh|ryP MWPTRW5ITVJ?
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8-MG-BA M3\Uemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTWb|dlUUN3ME22MlUyPTB5IN88US=> MV;TRW5ITVJ?
GT3TKB MoG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLa[3AxUUN3ME22MlYxPzZ|IN88US=> M3;1b3NCVkeHUh?=
KU812 M4XWUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPYfJNKSzVyPU[uOlk1OiEQvF2= MYTTRW5ITVJ?
CESS MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7PRWtTUUN3ME23MlExPDN6IN88US=> M4f6fXNCVkeHUh?=
BC-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEO5VmxKSzVyPUeuNlQ5OTJizszN NYexXFExW0GQR1XS
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NCI-H82 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnPSnBKSzVyPUeuN|c5PSEQvF2= NEOxR4pUSU6JRWK=
NCI-H1355 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PtXWlEPTB;Nz60OVgxPCEQvF2= NGPOWm9USU6JRWK=
RPMI-8226 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4[3N2lEPTB;Nz61NFc{QSEQvF2= NGXDboJUSU6JRWK=
ARH-77 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jzV2lEPTB;Nz61N|U6PyEQvF2= Mlr0V2FPT0WU
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IMR-5 M3H5Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\kV2lEPTB;N{C1OFg4PiEQvF2= MmSwV2FPT0WU
KARPAS-422 NUCxSnd1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTdwNUeyNFYh|ryP M1Tye3NCVkeHUh?=
CA46 M3;Zemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;5U2lEPTB;Nz61PFAyOiEQvF2= NGTROIVUSU6JRWK=
SJSA-1 NUTWRWZ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknMTWM2OD15Lk[2NFYyKM7:TR?= NH3EVoNUSU6JRWK=
no-11 M364S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;wem5KSzVyPUeuO|c2PTdizszN MoG1V2FPT0WU
IST-SL1 M4rGZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;RfIJKSzVyPUiuNFI1OTdizszN MYHTRW5ITVJ?
NCI-H209 M3q4VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRThwMUG2OVIh|ryP Mn7UV2FPT0WU
TALL-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7kVJVKSzVyPUiuNVg{QDRizszN MkHDV2FPT0WU
KMOE-2 M3vkeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHXTWM2OD16LkG5OFIh|ryP M1rHXnNCVkeHUh?=
HCC1599 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnGTWM2OD16LkG5PVg4KM7:TR?= NVG5eXgzW0GQR1XS
CI-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHvVoxFUUN3ME24MlIxPDFzIN88US=> NFW3fZhUSU6JRWK=
NCI-H1304 NIXZTmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRThwMkC2OlEh|ryP NV7PSo4zW0GQR1XS
Daudi MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrBRnVIUUN3ME24MlI{PTR4IN88US=> NV\YeY9bW0GQR1XS
CPC-N NFLKSYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrxTWM2OD16LkK5NVk6KM7:TR?= M2q3VHNCVkeHUh?=
MC-CAR M1XlfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjCcFhKSzVyPUiuN|M2QCEQvF2= NIPIWpJUSU6JRWK=
SW872 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELXV29KSzVyPUiuN|Q4PThizszN MnPpV2FPT0WU
OVCAR-4 MmHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEX0bI5KSzVyPUiuOVA{PTFizszN NHT3fXpUSU6JRWK=
OCUB-M MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRThwNU[1NFgh|ryP NIn0S2dUSU6JRWK=
SK-PN-DW MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRThwNkC5PFUh|ryP M2m4RXNCVkeHUh?=
NCCIT MmWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml[wTWM2OD16LkexO|Q2KM7:TR?= MlvjV2FPT0WU
NCI-H1648 Mnn0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;kSmlEPTB;OT6xN|g{PCEQvF2= MYLTRW5ITVJ?
COR-L279 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTkTmdtUUN3ME25MlM6ODlizszN M3\vbHNCVkeHUh?=
LS-123 MoW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\wTWM2OD17Lk[4NVYyKM7:TR?= MYXTRW5ITVJ?
LP-1 NFXGfHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrreIhKSzVyPUmuO|gxQDNizszN NFrrSGJUSU6JRWK=
NB13 NH7yTWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTlwN{m5PVQh|ryP MWrTRW5ITVJ?
ONS-76 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGT0Z3BKSzVyPUmuPFExOTZizszN MnjtV2FPT0WU
VA-ES-BJ M3nNfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXUUWFKSzVyPUmuPVk6OzNizszN NEXNfFlUSU6JRWK=
GR-ST MonIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFL1Uo5KSzVyPUGwMlIzODdizszN NYGzT2lIW0GQR1XS
ES1 Mn3RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;jcYdmUUN3ME2xNE4zQTh2IN88US=> MXrTRW5ITVJ?
NB14 NWjv[pRmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jLbGlEPTB;MUCuPVI4PyEQvF2= NHvZNIVUSU6JRWK=
Ramos-2G6-4C10 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTFzLkK2OUDPxE1? MXzTRW5ITVJ?
RXF393 NF[ydW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvWTWM2OD1zMT60PFM1KM7:TR?= MkHRV2FPT0WU
NCI-H2107 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3O1OmlEPTB;MUGuOVk5PCEQvF2= M4\Sc3NCVkeHUh?=
K562 MlruS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mor3TWM2OD1zMT64O|AzKM7:TR?= NWfyd21SW0GQR1XS
LOUCY MmO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PZOWlEPTB;MUGuPVg4PSEQvF2= M2\x[XNCVkeHUh?=
TGBC1TKB NV3mcGtTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnK1TWM2OD1zMj6wNFIh|ryP M4fFXXNCVkeHUh?=
COLO-320-HSR MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXUc2lMUUN3ME2xNk4yPTZ3IN88US=> MVHTRW5ITVJ?
K5 Mn33S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTF{LkK5PFUh|ryP Mn7vV2FPT0WU
BC-3 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmKzTWM2OD1zMj60OlUyKM7:TR?= MmrJV2FPT0WU
REH NHjGNoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF65OIlKSzVyPUGyMlY1QThizszN MYHTRW5ITVJ?
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NCI-H128 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml24TWM2OD1zMz6wO|I{KM7:TR?= MkS2V2FPT0WU
NCI-H1694 NEjudG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTF|LkGxOFQh|ryP NXT6OGhiW0GQR1XS
TGW NHPqe5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnPTWM2OD1zMz6zNlc3KM7:TR?= NG[3d49USU6JRWK=
NCI-SNU-1 MkLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nFRWlEPTB;MUOuN|Q2KM7:TR?= NWnXUI1xW0GQR1XS
IST-MES1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfhUVV{UUN3ME2xN{43PzJ7IN88US=> M{fjcXNCVkeHUh?=
CTB-1 M3S0bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33uWmlEPTB;MUOuO|I6PCEQvF2= NFrWNnhUSU6JRWK=
HUTU-80 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1G1cWlEPTB;MUOuO|U4OyEQvF2= M{nwfHNCVkeHUh?=
LAN-6 MmjvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPYd3JKSzVyPUG0MlI1PTdizszN M4i4fXNCVkeHUh?=
KP-N-YS M1HKNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7sTWM2OD1zND6yPFk1KM7:TR?= NILOb3JUSU6JRWK=
CCRF-CEM NHXQUIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIK1TYxKSzVyPUG0MlQyPjlizszN M3T0UnNCVkeHUh?=
NCI-H1770 Mmf6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{T3W2lEPTB;MUSuOVM3QSEQvF2= MUnTRW5ITVJ?
MZ2-MEL MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\yWmlEPTB;MUWuNlI2OSEQvF2= NUD3ZYVqW0GQR1XS
COR-L88 Ml31S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTF4LkCwNVIh|ryP MV\TRW5ITVJ?
LOXIMVI M3LYW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;qXGlEPTB;MU[uNlU3KM7:TR?= MVXTRW5ITVJ?
KALS-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTF4LkW5N|Eh|ryP MXXTRW5ITVJ?
D-283MED NF\zOWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DDVGlEPTB;MU[uPFQ5QSEQvF2= MVHTRW5ITVJ?
NCI-H719 M17YO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\LO49KSzVyPUG2MlkyPjFizszN MlOwV2FPT0WU
MLMA MlzQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XmbGlEPTB;MU[uPVkxPyEQvF2= M2qyWXNCVkeHUh?=
EVSA-T MlnhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTF5LkC0PFUh|ryP MoLaV2FPT0WU
SK-N-FI NXW4XppUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPBTWM2OD1zNz62PVE{KM7:TR?= NEfiO|NUSU6JRWK=
NTERA-S-cl-D1 NH7GVZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTF5Lki1O|Ih|ryP M{GxeXNCVkeHUh?=
NCI-H1882 NFfJS|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjtNmJKSzVyPUG3Mlk5OzRizszN NXT5cZhQW0GQR1XS
A704 MmnRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3z[ZdKSzVyPUG3Mlk6ODRizszN NYn4PIF{W0GQR1XS
L-428 Ml;aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIm1Z3JKSzVyPUG4MlAyPTFizszN MoHHV2FPT0WU
HCC1187 MlvoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrF[lh1UUN3ME2xPE4xOTh5IN88US=> NGrSSm1USU6JRWK=
NCI-H1581 NUP5[|VXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{H1PGlEPTB;MUiuNFg3PiEQvF2= M{PPRnNCVkeHUh?=
BB65-RCC NFnIUoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTF6LkSxOlIh|ryP MnLXV2FPT0WU
EM-2 M2O0[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTF6LkW2O|Ih|ryP NW\i[pdyW0GQR1XS
Raji NV\SWVU2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTF7Lkm1OlUh|ryP MUjTRW5ITVJ?
TE-1 M3nCcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWK2XIZ1UUN3ME2yNE41OTB2IN88US=> NWXEOXo3W0GQR1XS
SW962 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrwSIlnUUN3ME2yNE41Ojl|IN88US=> MmjOV2FPT0WU
MHH-NB-11 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnznTWM2OD1{MD61OVIyKM7:TR?= NWXHc4kyW0GQR1XS
no-10 NFXxVJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTJzLkCyOlQh|ryP MXLTRW5ITVJ?
GDM-1 NWDZcmg2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX64[ZF3UUN3ME2yNU46PDF2IN88US=> MVHTRW5ITVJ?
KMS-12-PE NIHxXYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nMdGlEPTB;MkKuNlc1KM7:TR?= NHn3e3pUSU6JRWK=
NCI-H510A NFH4[G9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PJd2lEPTB;MkSuNVI4QCEQvF2= M1;OeHNCVkeHUh?=
ES5 NEWycGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfze3VKSzVyPUK0Mlc{PDlizszN MorQV2FPT0WU
JiyoyeP-2003 NYj0bIVnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkH1TWM2OD1{Nj6yO|QzKM7:TR?= NHPLfJhUSU6JRWK=
NMC-G1 NFfqcW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;ONpZKSzVyPUK3MlE5OjJizszN MYfTRW5ITVJ?
NCI-H446 NYrCVZY6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFiw[FJKSzVyPUK3MlQ6PDZizszN M1\rfnNCVkeHUh?=
NB7 M1HNcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTJ5LkmyNlkh|ryP NVvEfFhoW0GQR1XS
A388 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITRUWtKSzVyPUK4MlAxPzRizszN M1fWPXNCVkeHUh?=
JVM-2 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\qO5I3UUN3ME2yPE4zQDl6IN88US=> NX;wRYNSW0GQR1XS
HT-144 NHn4TFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17a[mlEPTB;MkiuOlkh|ryP Ml7iV2FPT0WU
NCI-H747 MoXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XMd2lEPTB;MkiuPVE6PSEQvF2= MoXnV2FPT0WU
NCI-H1650 MoPSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnFTo1KSzVyPUK5MlAyPzZizszN NF:3ZlhUSU6JRWK=
EB-3 NIHrfJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HhVWlEPTB;MkmuOVMxQSEQvF2= NEfBU4dUSU6JRWK=
KLE M2izW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGCw[XZKSzVyPUK5MlYyQSEQvF2= MkO2V2FPT0WU
TK10 NGPFSXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlS3TWM2OD1|MD6xNlYh|ryP MWnTRW5ITVJ?
COLO-668 NEW4TpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{W3NGlEPTB;M{CuO|kzKM7:TR?= Ml;hV2FPT0WU
NCI-H23 M3SyO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\memlEPTB;M{GuNVA3OyEQvF2= NV6ydWkxW0GQR1XS
GOTO MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\OR|dKSzVyPUOxMlYxQDVizszN Mne2V2FPT0WU
MSTO-211H NXnFfIJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1W4cGlEPTB;M{GuPFY4QCEQvF2= MW\TRW5ITVJ?
LB831-BLC MknrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;vW2p3UUN3ME2zNk4{QDR|IN88US=> MXfTRW5ITVJ?
SCH NW\JUW5ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDaNYFKSzVyPUOyMlg1QDVizszN M1HIU3NCVkeHUh?=
EHEB NGHzUVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPQ[4FKSzVyPUO0MlEyQTNizszN MVfTRW5ITVJ?
U-266 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfoXod2UUN3ME2zOE4zPzhzIN88US=> NHrQNXlUSU6JRWK=
EW-11 Ml:0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7uXFRKSzVyPUO0MlQ4OjVizszN MV\TRW5ITVJ?
TE-9 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUj4TnZqUUN3ME2zO{4xPDBzIN88US=> MoPPV2FPT0WU
ES3 NIDmOlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTN5LkWwNFQh|ryP M3uzWnNCVkeHUh?=
NCI-H2141 NGm5S25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fGWmlEPTB;M{iuNFg1OyEQvF2= M4LhO3NCVkeHUh?=
MPP-89 NF7EcodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTs[YhKSzVyPUSyMlA2QDZizszN MXvTRW5ITVJ?
SK-MEL-2 M{nh[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrqTWM2OD12Mj62OFA2KM7:TR?= NY\V[WxqW0GQR1XS
LC-1F NWDHVod4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorqTWM2OD12Mz6zOlgzKM7:TR?= NVnTTYxJW0GQR1XS
NH-12 MnW3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLwdYZKSzVyPUSzMlk{PTlizszN NYrBfnBNW0GQR1XS
RKO NYHmW3NVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTR2LkGyOVIh|ryP Mn;aV2FPT0WU
KM-H2 M1;scWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4WwVmlEPTB;NESuPVU4PyEQvF2= M2fMTHNCVkeHUh?=
SK-UT-1 NVPzfnpXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlO1TWM2OD12OT64PFI2KM7:TR?= NHK4b25USU6JRWK=

... Click to View More Cell Line Experimental Data

In vivo Consistent with the substantial and selective inhibition of VEGFR2 or PDGFR phosphorylation and signaling in vivo, Sunitinib (20-80 mg/kg/day) exhibits broad and potent dose-dependent anti-tumor activity against a variety of tumor xenograft models including HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435. Sunitinib dosing at 80 mg/kg/day for 21 days leads to complete tumor regression in six of eight mice, without tumor re-growing during a 110-day observation period after the end of treatment. Second round of treatment with Sunitinib remains efficacious against tumors that are not fully regressed during the first round of treatment. Sunitinib treatment results in significant decrease in tumor MVD, with ~40% reduction in SF763T glioma tumors. SU11248 treatment results in a complete inhibition of additional tumor growth of luciferase-expressing PC-3M xenografts, despite no reduction in tumor size. [2] Sunitinib treatment (20 mg/kg/day) dramatically suppresses the growth subcutaneous MV4;11 (FLT3-ITD) xenografts and prolongs survival in the FLT3-ITD bone marrow engraftment model. [3]

Protocol

Kinase Assay:[1]
+ Expand

Biochemical Tyrosine Kinase Assays:

IC50 values for Sunitinib against VEGFR2 (Flk-1) and PDGFRβ are determined using glutathione S-transferasefusion proteins containing the complete cytoplasmic domain of the RTK. Biochemical tyrosine kinase assays to quantitate the trans-phosphorylation activity of VEGFR2 (Flk-1) and PDGFRβ are performed in 96-well microtiter plates precoated (20 μg/well in PBS; incubated overnight at 4 °C) with the peptide substrate poly-Glu,Tyr (4:1). Excess protein binding sites are blocked with the addition of 1-5% (w/v) BSA in PBS. Purified GST-fusion proteins are produced in baculovirus-infected insect cells. GST-VEGFR2 and GST-PDGFRβ are then added to the microtiter wells in 2 × concentration kinase dilution buffer consisting of 100 mM HEPES, 50 mM NaCl, 40 μM NaVO4, and 0.02% (w/v) BSA. The final enzyme concentration for GST-VEGFR2 or GST-PDGFRβ is 50 ng/mL. Twenty-five μL of diluted Sunitinib are subsequently added to each reaction well to produce a range of inhibitor concentrations appropriate for each enzyme. The kinase reaction is initiated by the addition of different concentrations of ATP in a solution of MnCl2 so that the final ATP concentrations spanned the Km for the enzyme, and the final concentration of MnCl2 is 10 mM. The plates are incubated for 5-15 minutes at room temperature before stopping the reaction with the addition of EDTA. The plates are then washed three times with TBST. Rabbit polyclonal antiphosphotyrosine antisera are added to the wells at a 1:10,000 dilution in TBST containing 0.5% (w/v) BSA, 0.025% (w/v) nonfat dry milk, and 100 μM NaVO4 and incubated for 1 hour at 37 °C. The plates are then washed three times with TBST, followed by the addition of goat antirabbit antisera conjugated with horseradish peroxidase (1:10,000 dilution in TBST). The plates are incubated for 1 hour at 37 °C and then washed three times with TBST. The amount of phosphotyrosine in each well is quantitated after the addition of 2,2′-azino-di-[3-ethylbenzthiazoline sulfonate] as substrate.
Cell Research:[3]
+ Expand
  • Cell lines: RS4;11, MV4;11, and OC1-AML5
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 24 and 48 hours
  • Method: Cells are starved overnight in medium containing 0.1% FBS prior to addition of Sunitinib and FL (50 ng/mL; FLT3-WT cells only). Proliferation is measured after 48 hours of culture using the Alamar Blue assay or trypan blue cell viability assays. Apoptosis is measured 24 hours after Sunitinib addition by Western blotting to detect cleavage of poly (ADP-ribose) polymerase (PARP) or levels of caspase-3.
    (Only for Reference)
Animal Research:[2]
+ Expand
  • Animal Models: Female nu/nu mice implanted s.c. with HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435, and male nu/nu mice bearing luciferase-expressing PC-3M tumors
  • Formulation: Formulated as a carboxymethyl cellulose suspension or as a citrate buffered (pH 3.5) solution
  • Dosages: ~80 mg/kg
  • Administration: Orally once daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 15 mg/mL (28.16 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 4% DMSO+30% PEG 300+ddH2O 2mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 532.56
Formula

C22H27FN4O2.C4H6O5

CAS No. 341031-54-7
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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Molecular Weight Calculator

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02761057 Recruiting Recurrent Renal Cell Carcinoma|Stage III Renal Cell Cancer|Stage IV Renal Cell Cancer|Type 1 Papillary Renal Cell Carcinoma|Type 2 Papillary Renal Cell Carcinoma National Cancer Institute (NCI) April 2016 Phase 2
NCT02779283 Recruiting Untreated Adult Acute Myeloid Leukemia OHSU Knight Cancer Institute|National Cancer Institute (NCI) December 2015 Phase 1
NCT02626754 Enrolling by invitation Renal Cell Carcinoma vghtpe user|Taipei Veterans General Hospital, Taiwan August 2015 Phase 2
NCT02465060 Recruiting Advanced Malignant Neoplasm|Lymphoma|Recurrent Plasma Cell Myeloma|Recurrent Solid Neoplasm|Refractory Malignant Neoplasm|Refractory Plasma Cell Myeloma National Cancer Institute (NCI) August 2015 Phase 2
NCT01835158 Active, not recruiting Clear Cell Renal Cell Carcinoma|Metastatic Renal Cell Cancer|Stage III Renal Cell Cancer|Stage IV Renal Cell Cancer National Cancer Institute (NCI) July 2013 Phase 2
NCT01740154 Terminated Fatigue|Recurrent Renal Cell Cancer|Stage IV Renal Cell Cancer Case Comprehensive Cancer Center|National Cancer Institute (NCI) September 2012 --

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID